General description

Suramin is an antiparasitic drug, which blocks endothelial cell proliferation and increases tyrosine phosphorylation of many signalling proteins. It is associated with urticaria, paresthesias, vomiting and neurologic toxicity. Suramin is used to treat trypanosomiasis and onchocerciasis. It functions as an inhibitor of heparanase and also exhibits anti-AIDS (acquired immunodeficiency syndrome) property.

Application

Suramin sodium salt has been used:

as a potent blocker of rat P2Y₂ purinergic receptor
to study its effects on short circuit current (I_sc) across strial marginal cells
to show its effects on initial burst of glial activity
to assess its neuroprotective potential in rats
as a purinoceptor inhibitor, to explore the mechanism of action of extracellular adenosine triphosphate (eATP)

Biochem/physiol Actions

Suramin is a polysulfonated naphthylurea anticancer agent that inhibits tumor cell proliferation. It inhibits the activity of topoisomerase II by blocking the binding of the enzyme to DNA. It′s antiangiogenic activity may be related to its ability to bind to and inhibit the activity of several growth factors, including FGFa, FGFb, and PGDF. It uncouples G-proteins from receptors. It is an broad spectrum antagonist at P2X and P2Y purinergic receptors. Suramin has well documented antiprotozoal and anthelmintic activity.

Other Notes

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